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endocrine drugs
| Question | Answer |
|---|---|
| Inhibitor of Na+-I- cotransporter | PERCHLORATE |
| mechanism and main toxicity of perchlorate | Block uptake of iodide (I-), Aplastic Anemia |
| Iodide mechanism | Inhibit organification, Inhibit release of T3 and T4 (via inhibition of proteases), decrease size and vascularity of gland |
| Radioactive Iodine (131I) mechanism | Rapid uptake of Iodine, Emission of radioactive β-particle Selective destruction of thyroid tissue |
| how toxic is radio active Iodine | little to no toxicity |
| PROPYLTHIOURACIL (PTU) mechanism | Block Organification, inhibit thyroid peroxidase |
| PROPYLTHIOURACIL is a | Thioamide |
| Levothyroxine is | t4 analogue |
| Ketoconazole is | an antifungal |
| ketoconazole mechanism | a non-selective inhibitor of steroid hormone biosynthesis. It inhibits various enzymes in the biosynthetic pathway of cortisol |
| Ketoconazole interacts with | statins ex: simvastatin |
| Mifepristone | GC receptor antagonist |
| Mitotane | chemically non-selective adrenalectomic agent |
| OXYTOCIN actions | Induces contraction of smooth muscle in reproductive tracts, initiating labor, stimulates lactation |
| DESMOPRESSIN ACETATE is | a long synthetic vasopressin anologue, it has minimal vasoconstrictor effects. The Antidiuretic : Pressor ratio is 4000x higher than native ADH |
| CONIVAPTAN is | ADH ANTAGONISTS: Used in patients with hyponatremia or acute HF. It has a high affinity for V1A and V2 rec |
| Chloropromide and Glyburide desctiption and MOA | its a Sulfonylurea, which inhibits the atpase sensitive k channel |
| Chloropromide and Glyburide effect | INCREASE insulin release from pancreas DECREASE Glucagon levels (mechanism unclear) |
| Chloropromide and Glyburide TOXICITY/SIDE EFFECTS | Hypoglycemia (Most common side effect) Weight Gain Potentially Teratogenic |
| PRAMLINITIDE is | Amylin Analog, a synthetic human amylin |
| MOA and effects | Binds to the Amylin Receptor in specific regions of the brain. Activation of the amylin receptor cause reductions in glucagon release Promotes satiety, slows gastric emptying |
| PRAMLINITIDE Drug-Drug Interaction | Contraindicated in patients with disorders of motility or on drugs that decrease gastric motility (i.e. OPIODE ANALGESICS) |
| REPAGLINIDE is | Meglitinides |
| REPAGLINIDE MOA | STIMULATE insulin release from pancreas Similar mechanism to sulfonylureas |
| NATEGLINIDE is | d-phenylalanine derivative |
| NATEGLINIDE MOA | STIMULATE insulin release from pancreas Similar mechanism to sulfonylureas |
| NATEGLINIDE and REPAGLINIDE adverse effects | Hypoglycemia, diarrhea, nausea and weight gain |
| Metformin is a | Biguanide that activates ampk |
| METFORMIN effects | Liver: Decreases gluconeogenesis Skeletal muscle: Increase glucose utilization (lowers glucose levels) DOES NOT DEPEND ON FUNCTIONING PANCREATIC BETA CELLS |
| Metformin adverse effects and metabolism | IMPAIRS HEPATIC LACTIC ACID METABOLISM Lactic acidosis Muscle pain Metabolism: Not metabolized Excreted unchanged in the urine |
| PIOGLITAZONE | Insulin Sensitizer: Thiazolidinediones (TZD’s) |
| PIOGLITAZONE MOA | acts on PPAR GAMMA INCREASE INSULIN SENSITIVITY DECREASE INSULIN RESISTANCE INCREASE GLUCOSE UTILIZATION |
| PIOGLITAZONE adverse effects | ASSOCIATED WITH BLADDER CANCER FLUID RETENTION |
| ACARBOSE | ALPHA-GLUCISIDASE INHIBITOR |
| ACARBOSE MOA | Inhibit α-glucosidase in GI tract Decrease absorption of Glucose |
| Acarbose | GI disturbance Excess carbohydrates in GI tract lead to increased bacterial digestion of polysaccharides. Contraindicated in people with Inflammatory Bowel Disease |
| EXENATIDE | GLUCAGON-LIKE PEPTIDE-1 (GLP-1) RECEPTOR AGONISTS |
| EXENATIDE effects | promotes: STIMULATES INSULIN PRODUCTION REDUCES APPETITE INDUCES β-CELL GROWTH |
| EXENATIDE adverse effects | GI disturbance |
| SITAGLIPTIN | DIPEPTIDYL PEPTIDASE-4 (DPP-4) INHIBITOR |
| sitagliptin effects | INCREASE CIRCULATING GLP-1 INCREASE INSULIN LEVCELS DECREASE GLUCAGON LEVELS Adverse effects: GI disturbance |
| CANAGLIFLOZIN | Sodium-Glucose transporter inhibitor (SGLT-2 inhibitor) |
| Canagliflozin MOA | Inhibits the reabsorbtion of glucose Results in loss of glucose (glycosuria) and water (osmotic diuresis) |
| Canagliflozin Adverse effects | Increased urination Increased urinary tract infections Possible hypotension |
| SIMVASTATIN is | a prodrug, absorbed in the small intestine, and activated in the liver |
| DRUGS THAT INTERFERE WITH STATIN OXIDATION | Macrolide antibiotics: e.g. Erythromycin Azole antifungals: e.g. Itraconazole Cyclosporine (immunosuppressant) Nefazodone (a phenylpiperazine antidepressant) HIV protease inhibitors Amiodarone (Antiarrhythmic agent) |
| Adverse effects of statins (simvastatin) | MYOPATHY The major adverse effect associated with statin use Statin-induced rhabdomyolysis Risk increased in proportion to dose and plasma concentrations Associated with factors inhibiting statin catabolism |
| CHOLESTYRAMINE | Bile-Acid Sequestrant |
| CHOLESTYRAMINE MOA | Positively charged compounds IONIC BOND with negatively charged bile acids Block reabsorbtion and enhance excretion of cholesterol ENHANCES bile acid synthesis reduces hepatic cholesterol → INC LDL-R synthesis |
| CHOLESTYRAMINE adverse | Relatively safe Interfere with absorption of other drugs FUROSEMIDE, THIAZIDE DIURETICS,PROPRANOLOL, DIGOXIN, WARFARIN |
| niacin MOA | Inhibits hormone-sensitive lipase DECREASES hepatic TG synthesis Decreases VLDL production and release Decreases HDL breakdown |
| Niacin ADVERSE EFFECTS | Cutaneous vasodilation (flush) A prostaglandin dependent phenomena Treated with NSAIDs, salicylate-containing creams (i.e. Aspercreme™) and aspirin Dyspepsia May increase insulin resistance |
| CLOFIBRATE MOA | Act as PPARα ligands |
| Clofibrate effects | Increased FFA OXIDATION Increased expression and release of ApoA1 INC expression of LPL ↓ HEPATIC VLDL SECRETION, ↓ TGs, modest ↓ LDL, ↑ HDL |
| Clofibrate adverse effects | Displace oral anticoagulants from protein binding sites. Myopathy when combined w/ statins (gemfibrozil only) Gemfibrozil blocks OATP1B1 transporter Associated w/ gallstone formation |
| EZETIMIBE MOA | Inhibits luminal cholesterol uptake in the SMALL INTESTINE Decreases cholesterol uptake into chylomicrons Reduces cholesterol in liver Increases LDL-Receptor expression Inc plasma LDL clearance |
| Ezetimibe interactions | BILE ACID SEQUESTRANTS INHIBIT ABSORBTION (ex: cholestyramine) CONTRAINDICATED No other interaction reported |
| ALIROCUMAB is | a pcsk9 inhibitor. ( PCSK9 inhibitors have been shown to reduce LDL levels by up to 60 percent from baseline levels, (including in statin-intolerant) |
| ALIROCUMAB MOA | Binds and inactivates PCSK9 Inhibits degradation of LDL-R Increases LDL-R number |
| ALIROCUMAB adverse effect | Itching and swelling at site of injection Flu-like symptoms Hypersensitivity-type reactions |
| Somatotropin | is Identical to human GH |
| Mecasermin | recombinant human IGF-I (rh IGF-I) - Used for treatment of GH-resistant IGF-I deficiency |
| Octreotide | Somatostatin analog |
| Pegvisomant | GH receptor anatgonist, Binds only to one GH receptor, will stop dimerization |
Created by:
ksoul6
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